Assay Detail
Binding
CHEMBL1104358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRAF V600E mutant ERK phosphorylation in human WM266.4 cells
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | WM266.4 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 6.35 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090975 | — | — | 1 | 7.85 |
| CHEMBL1090977 | — | — | 1 | 7.72 |
| CHEMBL1090979 | — | — | 1 | 7.58 |
| CHEMBL1090980 | — | — | 1 | 7.57 |
| CHEMBL1093756 | — | — | 1 | 7.46 |
| CHEMBL1090976 | — | — | 1 | 7.46 |
| CHEMBL1090289 | — | — | 1 | 7.44 |
| CHEMBL1091849 | — | — | 1 | 7.40 |
| CHEMBL1092540 | — | — | 1 | 7.28 |
| CHEMBL1091430 | — | — | 1 | 7.27 |
| CHEMBL1092541 | — | — | 1 | 7.25 |
| CHEMBL1092183 | — | — | 1 | 7.21 |
| CHEMBL1090705 | — | — | 1 | 7.16 |
| CHEMBL1090981 | — | — | 1 | 7.16 |
| CHEMBL1089347 | — | — | 1 | 7.05 |
| CHEMBL1090978 | — | — | 1 | 7.00 |
| CHEMBL1092188 | — | — | 1 | 6.91 |
| CHEMBL1092771 | — | — | 1 | 6.89 |
| CHEMBL1090449 | — | — | 1 | 6.87 |
| CHEMBL1093364 | — | — | 1 | 6.79 |
| CHEMBL1091431 | — | — | 1 | 6.72 |
| CHEMBL1090290 | — | — | 1 | 6.69 |
| CHEMBL1090706 | — | — | 1 | 6.63 |
| CHEMBL1092464 | — | — | 1 | 6.46 |
| CHEMBL1093757 | — | — | 1 | 6.42 |
| CHEMBL1089003 | — | — | 1 | 6.39 |
| CHEMBL1092817 | — | — | 1 | 6.38 |
| CHEMBL1091039 | — | — | 1 | 6.33 |
| CHEMBL1092522 | — | — | 1 | 6.21 |
| CHEMBL1089014 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090975 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1090977 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1090979 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1090980 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1093756 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1090976 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1090289 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1091849 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1092540 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1091430 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1092541 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1092183 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1090705 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1090981 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1089347 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1090978 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1092188 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1092771 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1090449 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1093364 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL1091431 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1090290 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL1090706 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL1092464 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1093757 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL1089003 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL1092817 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1091039 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1092522 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1089014 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1089705 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL1093704 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL1092523 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL1091432 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1092770 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1093064 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1089704 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1089348 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL1090716 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL1093703 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1093065 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL1089706 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL1089349 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL1089691 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL1092465 | — | IC50 | = | 70000.0 | nM | 4.16 |